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Items: 1 to 50 of 119

1.

Structure-based and property-driven optimization of N-aryl imidazoles towards potent and selective oral RORγt inhibitors.

Hoegenauer K, Kallen J, Jimenez-Nunez E, Strang R, Ertl P, Cooke NG, Hintermann S, Voegtle M, Betschart C, Mckay DJJ, Wagner J, Ottl J, Beerli C, Billich A, Dawson J, Kaupmann K, Streiff M, Gobeau N, Harlfinger S, Stringer R, Guntermann C.

J Med Chem. 2019 Nov 15. doi: 10.1021/acs.jmedchem.9b01291. [Epub ahead of print]

PMID:
31729873
2.

Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.

Carcache DA, Vulpetti A, Kallen J, Mattes H, Orain D, Stringer R, Vangrevelinghe E, Wolf RM, Kaupmann K, Ottl J, Dawson J, Cooke NG, Hoegenauer K, Billich A, Wagner J, Guntermann C, Hintermann S.

J Med Chem. 2018 Aug 9;61(15):6724-6735. doi: 10.1021/acs.jmedchem.8b00529. Epub 2018 Jul 24.

PMID:
29990434
3.

Interferon regulatory factor 5 and nuclear factor kappa-B exhibit cooperating but also divergent roles in the regulation of pro-inflammatory cytokines important for the development of TH1 and TH17 responses.

Stein T, Wollschlegel A, Te H, Weiss J, Joshi K, Kinzel B, Billich A, Guntermann C, Lehmann JCU.

FEBS J. 2018 Aug;285(16):3097-3113. doi: 10.1111/febs.14600. Epub 2018 Jul 11.

4.

Pharmacological inhibition of RORγt suppresses the Th17 pathway and alleviates arthritis in vivo.

Guendisch U, Weiss J, Ecoeur F, Riker JC, Kaupmann K, Kallen J, Hintermann S, Orain D, Dawson J, Billich A, Guntermann C.

PLoS One. 2017 Nov 20;12(11):e0188391. doi: 10.1371/journal.pone.0188391. eCollection 2017.

5.

Feasibility and physiological relevance of designing highly potent aminopeptidase-sparing leukotriene A4 hydrolase inhibitors.

Numao S, Hasler F, Laguerre C, Srinivas H, Wack N, Jäger P, Schmid A, Osmont A, Röthlisberger P, Houguenade J, Bergsdorf C, Dawson J, Carte N, Hofmann A, Markert C, Hardaker L, Billich A, Wolf RM, Penno CA, Bollbuck B, Miltz W, Röhn TA.

Sci Rep. 2017 Oct 19;7(1):13591. doi: 10.1038/s41598-017-13490-1.

6.

Retinoic-acid-orphan-receptor-C inhibition suppresses Th17 cells and induces thymic aberrations.

Guntermann C, Piaia A, Hamel ML, Theil D, Rubic-Schneider T, Del Rio-Espinola A, Dong L, Billich A, Kaupmann K, Dawson J, Hoegenauer K, Orain D, Hintermann S, Stringer R, Patel DD, Doelemeyer A, Deurinck M, Schümann J.

JCI Insight. 2017 Mar 9;2(5):e91127. doi: 10.1172/jci.insight.91127.

7.

Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists.

Hintermann S, Guntermann C, Mattes H, Carcache DA, Wagner J, Vulpetti A, Billich A, Dawson J, Kaupmann K, Kallen J, Stringer R, Orain D.

ChemMedChem. 2016 Dec 16;11(24):2640-2648. doi: 10.1002/cmdc.201600500. Epub 2016 Nov 30.

PMID:
27902884
8.

Sphingosine 1-Phosphate Produced by Sphingosine Kinase 2 Intrinsically Controls Platelet Aggregation In Vitro and In Vivo.

Urtz N, Gaertner F, von Bruehl ML, Chandraratne S, Rahimi F, Zhang L, Orban M, Barocke V, Beil J, Schubert I, Lorenz M, Legate KR, Huwiler A, Pfeilschifter JM, Beerli C, Ledieu D, Persohn E, Billich A, Baumruker T, Mederos y Schnitzler M, Massberg S.

Circ Res. 2015 Jul 31;117(4):376-87. doi: 10.1161/CIRCRESAHA.115.306901. Epub 2015 Jun 30.

PMID:
26129975
9.

Reduced Activity of Sphingosine-1-Phosphate Lyase Induces Podocyte-related Glomerular Proteinuria, Skin Irritation, and Platelet Activation.

Schümann J, Grevot A, Ledieu D, Wolf A, Schubart A, Piaia A, Sutter E, Côté S, Beerli C, Pognan F, Billich A, Moulin P, Walker UJ.

Toxicol Pathol. 2015 Jul;43(5):694-703. doi: 10.1177/0192623314565650. Epub 2015 Jan 27.

PMID:
25630683
10.

Orally active 7-substituted (4-benzylphthalazin-1-yl)-2-methylpiperazin-1-yl]nicotinonitriles as active-site inhibitors of sphingosine 1-phosphate lyase for the treatment of multiple sclerosis.

Weiler S, Braendlin N, Beerli C, Bergsdorf C, Schubart A, Srinivas H, Oberhauser B, Billich A.

J Med Chem. 2014 Jun 26;57(12):5074-84. doi: 10.1021/jm500338n. Epub 2014 May 21.

PMID:
24809814
11.

Second generation S1P pathway modulators: research strategies and clinical developments.

Bigaud M, Guerini D, Billich A, Bassilana F, Brinkmann V.

Biochim Biophys Acta. 2014 May;1841(5):745-58. doi: 10.1016/j.bbalip.2013.11.001. Epub 2013 Nov 12. Review.

PMID:
24239768
12.

PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling.

Cai X, Xu Y, Cheung AK, Tomlinson RC, Alcázar-Román A, Murphy L, Billich A, Zhang B, Feng Y, Klumpp M, Rondeau JM, Fazal AN, Wilson CJ, Myer V, Joberty G, Bouwmeester T, Labow MA, Finan PM, Porter JA, Ploegh HL, Baird D, De Camilli P, Tallarico JA, Huang Q.

Chem Biol. 2013 Jul 25;20(7):912-21. doi: 10.1016/j.chembiol.2013.05.010.

13.

Partial deficiency of sphingosine-1-phosphate lyase confers protection in experimental autoimmune encephalomyelitis.

Billich A, Baumruker T, Beerli C, Bigaud M, Bruns C, Calzascia T, Isken A, Kinzel B, Loetscher E, Metzler B, Mueller M, Nuesslein-Hildesheim B, Kleylein-Sohn B.

PLoS One. 2013;8(3):e59630. doi: 10.1371/journal.pone.0059630. Epub 2013 Mar 27.

14.

Assay to measure the secretion of sphingosine-1-phosphate from cells induced by S1P lyase inhibitors.

Loetscher E, Schneider K, Beerli C, Billich A.

Biochem Biophys Res Commun. 2013 Apr 12;433(3):345-8. doi: 10.1016/j.bbrc.2013.03.004. Epub 2013 Mar 14.

PMID:
23499842
15.

Pharmacological inhibition of stearoyl CoA desaturase in the skin induces atrophy of the sebaceous glands.

Meingassner JG, Aschauer H, Winiski AP, Dales N, Yowe D, Winther MD, Zhang Z, Stütz A, Billich A.

J Invest Dermatol. 2013 Aug;133(8):2091-4. doi: 10.1038/jid.2013.89. Epub 2013 Feb 27. No abstract available.

16.

Cellular assay for the characterization of sphingosine-1-phosphate lyase inhibitors.

Billich A, Beerli C, Bergmann R, Bruns C, Loetscher E.

Anal Biochem. 2013 Mar 15;434(2):247-53. doi: 10.1016/j.ab.2012.11.026. Epub 2012 Dec 13.

PMID:
23246729
17.

A novel role of sphingosine 1-phosphate receptor S1pr1 in mouse thrombopoiesis.

Zhang L, Orban M, Lorenz M, Barocke V, Braun D, Urtz N, Schulz C, von Brühl ML, Tirniceriu A, Gaertner F, Proia RL, Graf T, Bolz SS, Montanez E, Prinz M, Müller A, von Baumgarten L, Billich A, Sixt M, Fässler R, von Andrian UH, Junt T, Massberg S.

J Exp Med. 2012 Nov 19;209(12):2165-81. doi: 10.1084/jem.20121090. Epub 2012 Nov 12.

18.

BZM055, an iodinated radiotracer candidate for PET and SPECT imaging of myelin and FTY720 brain distribution.

Briard E, Orain D, Beerli C, Billich A, Streiff M, Bigaud M, Auberson YP.

ChemMedChem. 2011 Apr 4;6(4):667-77. doi: 10.1002/cmdc.201000477. Epub 2011 Jan 30.

PMID:
21280229
19.

Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis.

Brinkmann V, Billich A, Baumruker T, Heining P, Schmouder R, Francis G, Aradhye S, Burtin P.

Nat Rev Drug Discov. 2010 Nov;9(11):883-97. doi: 10.1038/nrd3248. Epub 2010 Oct 29. Review.

PMID:
21031003
20.

Ovalbumin-induced plasma interleukin-4 levels are reduced in ceramide kinase-deficient DO11.10 RAG1-/- mice.

Niwa S, Urtz N, Baumruker T, Billich A, Bornancin F.

Lipids Health Dis. 2010 Jan 6;9:1. doi: 10.1186/1476-511X-9-1.

21.

4,5,6-Trisubstituted piperidinones as conformationally restricted ceramide analogues: synthesis and evaluation as inhibitors of sphingosine and ceramide kinases and as NKT cell-stimulatory antigens.

Mathew T, Cavallari M, Billich A, Bornancin F, Nussbaumer P, De Libero G, Vasella A.

Chem Biodivers. 2009 Oct;6(10):1688-715. doi: 10.1002/cbdv.200900045.

PMID:
19842132
22.

Synthesis and evaluation of sphingolipid analogues: modification of the hydroxy group at C(1) of 7-oxasphingosine, and of the hydroxy group at C(1) and the amide group of 7-oxaceramides.

Mathew T, Billich A, Cavallari M, Bornancin F, Nussbaumer P, De Libero G, Vasella A.

Chem Biodivers. 2009 May;6(5):705-24. doi: 10.1002/cbdv.200900013.

PMID:
19479849
23.

Synthesis of 7-aza- and 7-thiasphingosines, and evaluation of their interaction with sphingosine kinases and with T-cells.

Mathew T, Billaud C, Billich A, Cavallari M, Nussbaumer P, De Libero G, Vasella A.

Chem Biodivers. 2009 May;6(5):725-38. doi: 10.1002/cbdv.200900039.

PMID:
19479838
24.

Efficient elimination of nonstoichiometric enzyme inhibitors from HTS hit lists.

Habig M, Blechschmidt A, Dressler S, Hess B, Patel V, Billich A, Ostermeier C, Beer D, Klumpp M.

J Biomol Screen. 2009 Jul;14(6):679-89. doi: 10.1177/1087057109336586. Epub 2009 May 21.

PMID:
19470716
25.

Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors.

Mullershausen F, Zecri F, Cetin C, Billich A, Guerini D, Seuwen K.

Nat Chem Biol. 2009 Jun;5(6):428-34. doi: 10.1038/nchembio.173. Erratum in: Nat Chem Biol. 2009 Dec;5(12):954.

PMID:
19430484
26.

Sphingosine kinase 1 is essential for proteinase-activated receptor-1 signalling in epithelial and endothelial cells.

Billich A, Urtz N, Reuschel R, Baumruker T.

Int J Biochem Cell Biol. 2009 Jul;41(7):1547-55. doi: 10.1016/j.biocel.2009.01.001. Epub 2009 Jan 8.

PMID:
19162217
27.

Sphingolipid metabolizing enzymes as novel therapeutic targets.

Billich A, Baumruker T.

Subcell Biochem. 2008;49:487-522. doi: 10.1007/978-1-4020-8831-5_19. Review.

PMID:
18751924
28.

Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor.

Graf C, Klumpp M, Habig M, Rovina P, Billich A, Baumruker T, Oberhauser B, Bornancin F.

Mol Pharmacol. 2008 Oct;74(4):925-32. doi: 10.1124/mol.108.048652. Epub 2008 Jul 8.

PMID:
18612076
29.

Binding of pimecrolimus and tacrolimus to skin and plasma proteins: implications for systemic exposure after topical application.

Weiss HM, Fresneau M, Moenius T, Stuetz A, Billich A.

Drug Metab Dispos. 2008 Sep;36(9):1812-8. doi: 10.1124/dmd.108.021915. Epub 2008 Jun 4.

PMID:
18524871
30.

GS-4104 Gilead Sciences Inc.

Billich A.

IDrugs. 1998 May;1(1):122-8.

PMID:
18465516
31.

Phosphorylation by sphingosine kinase 2 is essential for in vivo potency of FTY720 analogues.

Högenauer K, Billich A, Pally C, Streiff M, Wagner T, Welzenbach K, Nussbaumer P.

ChemMedChem. 2008 Jul;3(7):1027-9. doi: 10.1002/cmdc.200800037. No abstract available.

PMID:
18383466
32.

Neutropenia with impaired immune response to Streptococcus pneumoniae in ceramide kinase-deficient mice.

Graf C, Zemann B, Rovina P, Urtz N, Schanzer A, Reuschel R, Mechtcheriakova D, Müller M, Fischer E, Reichel C, Huber S, Dawson J, Meingassner JG, Billich A, Niwa S, Badegruber R, Van Veldhoven PP, Kinzel B, Baumruker T, Bornancin F.

J Immunol. 2008 Mar 1;180(5):3457-66.

33.

Synthesis and immobilization of erythro-C14-omega-aminosphingosine-1-phosphate as a potential tool for affinity chromatography.

Ullrich T, Ghobrial M, Peters C, Billich A, Guerini D, Nussbaumer P.

ChemMedChem. 2008 Feb;3(2):356-60.

PMID:
18000941
34.

Brain penetration of the oral immunomodulatory drug FTY720 and its phosphorylation in the central nervous system during experimental autoimmune encephalomyelitis: consequences for mode of action in multiple sclerosis.

Foster CA, Howard LM, Schweitzer A, Persohn E, Hiestand PC, Balatoni B, Reuschel R, Beerli C, Schwartz M, Billich A.

J Pharmacol Exp Ther. 2007 Nov;323(2):469-75. Epub 2007 Aug 6.

PMID:
17682127
35.

FTY720-phosphate is dephosphorylated by lipid phosphate phosphatase 3.

Mechtcheriakova D, Wlachos A, Sobanov J, Bornancin F, Zlabinger G, Baumruker T, Billich A.

FEBS Lett. 2007 Jun 26;581(16):3063-8. Epub 2007 Jun 4.

36.

FTY720, an immunomodulatory sphingolipid mimetic: translation of a novel mechanism into clinical benefit in multiple sclerosis.

Baumruker T, Billich A, Brinkmann V.

Expert Opin Investig Drugs. 2007 Mar;16(3):283-9. Review.

PMID:
17302523
37.

Normal neutrophil functions in sphingosine kinase type 1 and 2 knockout mice.

Zemann B, Urtz N, Reuschel R, Mechtcheriakova D, Bornancin F, Badegruber R, Baumruker T, Billich A.

Immunol Lett. 2007 Mar 15;109(1):56-63. Epub 2007 Jan 30.

PMID:
17292973
38.

Synthesis of borondipyrromethene (BODIPY)-labeled sphingosine derivatives by cross-metathesis reaction.

Peters C, Billich A, Ghobrial M, Högenauer K, Ullrich T, Nussbaumer P.

J Org Chem. 2007 Mar 2;72(5):1842-5. Epub 2007 Jan 24.

PMID:
17249735
40.

Sphingosine 1-phosphate phosphatase 2 is induced during inflammatory responses.

Mechtcheriakova D, Wlachos A, Sobanov J, Kopp T, Reuschel R, Bornancin F, Cai R, Zemann B, Urtz N, Stingl G, Zlabinger G, Woisetschläger M, Baumruker T, Billich A.

Cell Signal. 2007 Apr;19(4):748-60. Epub 2006 Sep 30.

PMID:
17113265
41.

Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.

Hanessian S, Charron G, Billich A, Guerini D.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):491-4. Epub 2006 Oct 10.

PMID:
17070046
42.

Effects of ceramide-1-phosphate on cultured cells: dependence on dodecane in the vehicle.

Tauzin L, Graf C, Sun M, Rovina P, Bouveyron N, Jaritz M, Winiski A, Hartmann N, Staedtler F, Billich A, Baumruker T, Zhang M, Bornancin F.

J Lipid Res. 2007 Jan;48(1):66-76. Epub 2006 Oct 3.

43.

A critical beta6-beta7 loop in the pleckstrin homology domain of ceramide kinase.

Rovina P, Jaritz M, Höfinger S, Graf C, Dévay P, Billich A, Baumruker T, Bornancin F.

Biochem J. 2006 Dec 1;400(2):255-65.

44.

NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studies.

Ettmayer P, Baumruker T, Guerini D, Mechtcheriakova D, Nussbaumer P, Streiff MB, Billich A.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):84-7. Epub 2005 Oct 19.

PMID:
16236505
45.

Sphingosine kinase type 2 is essential for lymphopenia induced by the immunomodulatory drug FTY720.

Zemann B, Kinzel B, Müller M, Reuschel R, Mechtcheriakova D, Urtz N, Bornancin F, Baumruker T, Billich A.

Blood. 2006 Feb 15;107(4):1454-8. Epub 2005 Oct 13.

PMID:
16223773
46.

Steroid sulfatase inhibitors: their potential in the therapy of breast cancer.

Nussbaumer P, Billich A.

Curr Med Chem Anticancer Agents. 2005 Sep;5(5):507-28. Review.

PMID:
16178776
47.

Pimecrolimus permeates less than tacrolimus through normal, inflamed, or corticosteroid-pretreated skin.

Meingassner JG, Aschauer H, Stuetz A, Billich A.

Exp Dermatol. 2005 Oct;14(10):752-7.

PMID:
16176283
48.

Amprenavir (Vertex Pharmaceuticals Inc).

Billich A.

IDrugs. 1999 May;2(5):466-82.

PMID:
16155850
49.

Basal and induced sphingosine kinase 1 activity in A549 carcinoma cells: function in cell survival and IL-1beta and TNF-alpha induced production of inflammatory mediators.

Billich A, Bornancin F, Mechtcheriakova D, Natt F, Huesken D, Baumruker T.

Cell Signal. 2005 Oct;17(10):1203-17. Epub 2005 Jan 18.

PMID:
16038795
50.

Novel cyclosporin derivatives featuring enhanced skin penetration despite increased molecular weight.

Billich A, Vyplel H, Grassberger M, Schmook FP, Steck A, Stuetz A.

Bioorg Med Chem. 2005 May 2;13(9):3157-67.

PMID:
15809151

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